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Chemical Structure| 2097381-85-4 Chemical Structure| 2097381-85-4

Structure of VH-298
CAS No.: 2097381-85-4

Chemical Structure| 2097381-85-4

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VH-298 is a highly affinity inhibitor of E3 ubiquitin ligase VHL inhibitor (Kd = 80-90 nM) which can block the interaction of VHL and HIF-α, thus initiating hypoxic response.

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Product Details of VH-298

CAS No. :2097381-85-4
Formula : C27H33N5O4S
M.W : 523.65
SMILES Code : O=C([C@H]1N(C([C@@H](NC(C2(C#N)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3
MDL No. :MFCD30742947
InChI Key :NDVQUNZCNAMROD-RZUBCFFCSA-N
Pubchem ID :122199236

Safety of VH-298

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • E3 Ligase

    VHL:80 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS cells 50 µM 16 hours Upregulated mRNA levels of HIF-target genes CA9 and GLUT1 Nat Commun. 2016 Nov 4;7:13312
HeLa cells 10 µM 2 hours Induced HIF-1α accumulation Nat Commun. 2016 Nov 4;7:13312
RCC4-HA-VHL cells 150 µM 24 hours Increased mRNA levels of EPO Nat Commun. 2016 Nov 4;7:13312
HFF cells 100 µM 24 hours Upregulated mRNA levels of HIF-target genes CA9 and GLUT1 Nat Commun. 2016 Nov 4;7:13312
CTL cells 100 µM 8 hours Upregulated GLUT1 protein levels Nat Commun. 2016 Nov 4;7:13312
Human umbilical vein endothelial cells (hUVEC) 0 µM, 10 µM, 30 µM, 100 µM, 200 µM 24 hours To evaluate the effect of VH-298 on angiogenesis. Results showed that 30 μM VH-298 significantly promoted angiogenesis, while high doses (100 μM and 200 μM) inhibited angiogenesis. J Diabetes Res. 2019 Feb 17;2019:1897174
Human foreskin fibroblasts (HFFs) 100 µM 24 hours To validate the effect of VH298 on increasing VHL protein levels in HFF cells. J Biol Chem. 2021 Aug;297(2):100910
Human foreskin fibroblasts (HFF) 100 µM 24 hours To validate the effect of VH298 on VHL protein levels in HFF cells, results showed that VH298 treatment increased VHL protein levels. J Biol Chem. 2021 Aug;297(2):100910
Rat fibroblasts (rFb) 0 µM, 10 µM, 30 µM, 100 µM, 200 µM 48 hours To evaluate the effect of VH-298 on cell proliferation. Results showed that 30 μM and 100 μM VH-298 significantly promoted cell proliferation. J Diabetes Res. 2019 Feb 17;2019:1897174
HeLa cells 50 µM 48 hours VH298 selectively promoted peroxisome degradation without affecting mitochondria, ER, or Golgi apparatus Molecules. 2024 Jan 18;29(2):482
HTERT RPE-1 cells 50 µM 48 hours VH298 significantly increased the number of red-only puncta, indicating enhanced peroxisome degradation Molecules. 2024 Jan 18;29(2):482

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Streptozotocin (STZ)-induced hyperglycaemic rat model Local injection 30 μM VH298 Every three days for 21 days To evaluate the effect of VH-298 on wound healing in hyperglycaemic rats. Results showed that VH-298 significantly accelerated wound healing, increased angiogenesis and collagen deposition. J Diabetes Res. 2019 Feb 17;2019:1897174

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.55mL

1.91mL

0.95mL

19.10mL

3.82mL

1.91mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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